CN108853312B - Polycinnamic alcohol external gel and preparation method thereof - Google Patents

Polycinnamic alcohol external gel and preparation method thereof Download PDF

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CN108853312B
CN108853312B CN201811113540.5A CN201811113540A CN108853312B CN 108853312 B CN108853312 B CN 108853312B CN 201811113540 A CN201811113540 A CN 201811113540A CN 108853312 B CN108853312 B CN 108853312B
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lauromacrogol
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CN108853312A (en
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杨军营
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Shaanxi Tianyu Pharmaceutical Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/896Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/886Aloeaceae (Aloe family), e.g. aloe vera
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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Abstract

The invention relates to a poly cinnamic alcohol external gel and a preparation method thereof, and the components comprise urea, poly cinnamic alcohol, aloe extract, benzalkonium chloride, sodium alginate, potassium sorbate, menthol, glycerol, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and purified water. The invention is characterized in that the lauromacrogol with the functions of quickly relieving itching and pain, diminishing inflammation and reducing swelling and the aloe extract with the functions of astringency and skin repair are combined, and the gel film form is adopted for treating 1-2 degree burns and scalds, mosquito bites and bruises; the traditional Chinese medicine composition can not treat burns and scalds and mosquito bites and the like at present, and similar anti-inflammatory products or related inventions do not appear at present.

Description

Polycinnamic alcohol external gel and preparation method thereof
Technical Field
The invention relates to the technical field of skin external preparations, in particular to a lauromacrogol external gel and a preparation method thereof.
Background
After the patient burns and scalds, the epidermis and the subcutaneous tissue are damaged in different degrees, and the wound surface has strong knife cutting pain; since the wound surface is directly exposed to the space, bacteria and virus infection inflammation is easily generated, and simultaneously, body fluid or blood is damaged and seeped out of the wound surface due to normal skin tissues. At present, all the ointments commonly used for treating scalds and burns are difficult to thoroughly achieve the purposes of immediately relieving pain, diminishing inflammation and inhibiting exudation. The pain of the patient is too much in the treatment process; the skin is slowly scabbed and easy to scar.
The skin allergy, red swelling, pain and extreme itching of local and peripheral skin of a patient caused by sunburn or mosquito bite are difficult to endure, and ointment, floral water and the like appearing in the current market hardly achieve the effects of immediately relieving itching and pain and quickly eliminating the red swelling.
How to timely and rapidly and thoroughly relieve the symptoms of pain, exudation, infection, skin allergy, pain, extreme itching and the like caused by sunburn and mosquito bites of the scald and burn patients is a difficult problem which is difficult to overcome in the treatment of the scald and burn at home and abroad at present.
Disclosure of Invention
The invention aims to provide a lauromacrogol external gel and a preparation method thereof, which are used as external drugs for treating burns, scalds, sunburn, bruises, mosquito bites and other diseases.
The technical scheme adopted by the invention is as follows:
the externally applied lauromacrogol gel is characterized in that:
the externally applied polycinnamol gel contains the active components of polycinnamol, urea and aloe extract.
The externally applied lauromacrogol gel comprises the following components in parts by weight:
3-6 parts of urea;
3-5 parts of lauromacrogol;
0.5-4 parts of aloe extract.
The externally applied lauromacrogol gel also comprises the following components in parts by weight:
0.1-0.4 part of benzalkonium chloride;
0.5-3 parts of sodium alginate;
0.1-0.4 part of potassium sorbate;
0.1-1 part of menthol;
5-15 parts of glycerol;
0.01-1.00 part of disodium hydrogen phosphate dodecahydrate;
0.01-1.00 part of dihydrate sodium dihydrogen phosphate;
the balance of purified water;
the total amount is 100 parts.
The preparation method of the externally applied lauromacrogol gel is characterized by comprising the following steps:
the method is realized by the following steps:
the method comprises the following steps: weighing lauromacrogol with formula ratio, adding 10-15 parts of water, heating to 60 deg.C for dissolving to obtain phase I;
step two: weighing sodium alginate and aloe extract according to the formula ratio, adding glycerol, stirring to uniformly disperse the components, adding 50-60 parts of water, stirring and dissolving to obtain phase II;
step three: weighing benzalkonium chloride, potassium sorbate, urea, menthol, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and 10-15 parts of water according to the formula ratio, and stirring for dissolving to obtain phase III;
step four: adding the phase III and the phase II into the phase I respectively, adding water to 100 parts, stirring uniformly, standing and filling.
The invention has the following advantages:
the invention is characterized in that the lauromacrogol with the functions of quickly relieving itching and pain, diminishing inflammation and reducing swelling and the aloe extract with the functions of astringency and skin repair are combined, and the gel film form is adopted for treating 1-2 degree burns and scalds, mosquito bites and bruises. The traditional medicine for treating burns, scalds and mosquito bites can not achieve the purpose. Similar therapeutic anti-inflammatory products or related inventions are not available at present.
Detailed Description
The present invention will be described in detail with reference to specific embodiments.
The invention relates to a poly-cinnamic alcohol external gel, which is an external medicine with special effect on 1-2 degree burn, scald, sunburn, scratch, mosquito bite and other diseases, and comprises the following components in parts by weight:
3-6 parts of urea;
3-5 parts of lauromacrogol;
0.5-4 parts of aloe extract;
0.1-0.4 part of benzalkonium chloride;
0.5-3 parts of sodium alginate;
0.1-0.4 part of potassium sorbate;
0.1-1 part of menthol;
5-15 parts of glycerol;
0.01-1.00 part of disodium hydrogen phosphate dodecahydrate;
0.01-1.00 part of dihydrate sodium dihydrogen phosphate;
the balance of purified water;
the total amount is 100 parts.
The preparation method of the externally applied lauromacrogol gel is characterized by comprising the following steps:
the method is realized by the following steps:
the method comprises the following steps: weighing lauromacrogol with formula ratio, adding 10-15 parts of water, heating to 60 deg.C for dissolving to obtain phase I;
step two: weighing sodium alginate and aloe extract according to the formula ratio, adding glycerol, stirring to uniformly disperse the components, adding 50-60 parts of water, stirring and dissolving to obtain phase II;
step three: weighing benzalkonium chloride, potassium sorbate, urea, menthol, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and 10-15 parts of water according to the formula ratio, and stirring for dissolving to obtain phase III;
step four: adding the phase III and the phase II into the phase I respectively, adding water to 100 parts, stirring uniformly, standing and filling.
The main active ingredients of the externally applied polycinnamol gel provided by the invention are polycinnamol, urea and an aloe extract. The lauromacrogol is an ether compound, is also named as ethoprosterol and polidocanol, is the most widely clinically applied sclerosant in European and American countries at present, is mainly applied to sclerotherapy of varicose veins, venous malformation, hemangioma, internal hemorrhoid, cystic disease and the like, is introduced into Germany for the first time in 1936 to be used as an anesthetic, and in 1963, Henschel finds that intravascular injection of high-concentration lauromacrogol has a vascular wall stimulation effect, and deeply researches on the lauromacrogol on the market, and reports the sclerotherapy effect of the lauromacrogol for the first time. 1967 Polycinnamic alcohol is used as hardener. In addition, the lauromacrogol also has a mild anesthetic effect, so the lauromacrogol serving as an external preparation not only can promote the rapid scabbing and healing of wounds, but also has the effects of rapidly relieving itching, relieving pain and the like, and can be used for treating mild skin burns and scalds, abrasions, sunburn, mosquito bites and the like.
Polycinnamic alcohol orally administered LD50 in rat at 1000mg/kg and LD50 orally administered mouse at 1170mg/kg has very little side effects and is used in cosmetic formulations.
Poly cinnamic alcohol:
chemical name: polyoxyethylene lauryl alcohol ether
English name: polidocanol
CAS number: 3055-99-0
Molecular weight: 582.8
Urea has the effects of moisturizing and softening cutin, so that it can also prevent cutin from blocking capillary pores, thereby improving the problem of acne. Can be used as moisture keeping component in facial mask, skin care lotion, cream, hand cream, etc.
Aloe has been used as a good medicine for treating burn and trauma for a long time in domestic and abroad, and the existing research shows that aloe has multiple functions of resisting inflammation, resisting oxygen free radicals, regulating immunity, resisting bacteria, resisting fungi, resisting viruses, resisting radiation, resisting cancers and the like. Meanwhile, the aloe extract also has the effects of nutrition, moisture retention, sun protection, inflammation resistance, skin repair and the like, and is commonly used for adding moisture retention components into products such as facial masks, creams, hand creams and the like; menthol has antipruritic, analgesic, antiseptic, irritant, anesthetic, refreshing and anti-inflammatory effects; benzalkonium chloride and potassium sorbate are used as antiseptic bactericide in medicine industry, and have antibacterial and wound infection preventing effects.
According to the fact that the lauromacrogol has a light anesthetic effect and can exert the effects of quickly relieving pain and itching after being externally used, the sodium alginate is added in combination with the treatment experience of the aloe extract and the menthol for mild burns and scalds, the viscosity of the gel matrix is increased, and the gel is coated on the surface of the skin in a film form, so that the injured skin can be protected from infection, secretion is facilitated to be discharged, and the medicine can exert various treatment effects. The combination of the two is used for treating burns, scalds, abrasions, sunburn, mosquito bites and the like, which is difficult to think by the ordinary skilled person. There is no patent description of similar products or products on the market after being inquired.
After the gel is applied to the surfaces of scalds and burns, a plurality of drug effects are immediately and directly generated on the wound surfaces, and the pharmacological action mechanism is as follows:
1. quick analgesic and antipruritic effects
The main component of the medicine, namely the lauromacrogol, has an anesthetic effect and can immediately relieve pain and itching.
2. Stopping bleeding and inhibiting exudation
The aloe extract has astringent effect and can inhibit exudation of secretion, and the lauromacrogol can rapidly exert capillary sclerosis effect to stop bleeding.
3. Controlling infection: after the gel is smeared on a wounded surface, potassium sorbate and benzalkonium chloride in the gel quickly have direct killing and inhibiting effects on various staphylococci, streptococci, various bacilli and viruses, and directly achieve the aims of resisting bacteria, diminishing inflammation and reducing swelling.
4. Promoting tissue regeneration and growing flesh, and recovering skin: after the gel is smeared on the wound surface, the aloe extract, the lauromacrogol and the urea can ensure that injured histiocytes can obtain enough blood nutrition in time, promote the hyperplasia of muscle cells to rapidly scab, simultaneously, according to the principle of physiological reprint regeneration of skin, the scabs fall off, the new skin has no appearance different from the original skin, no scar exists, and the wound surface is completely recovered.
EXAMPLE 1
[ FORMULATION ]
Figure BDA0001809890040000071
[ PREPARATION METHOD ]
1. Weighing lauromacrogol with formula ratio, adding 10g water, heating to 60 deg.C for dissolving to obtain phase I.
2. Weighing sodium alginate and aloe extract according to the formula ratio, adding 10g of glycerol, stirring to uniformly disperse the sodium alginate, adding 50g of water, and stirring to dissolve to obtain phase II.
3. Weighing urea, benzalkonium chloride, potassium sorbate, menthol, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and 10g of water according to the formula ratio, and stirring to dissolve to obtain phase III.
4. Respectively adding the first phase and the third phase into the second phase, stirring, adding water to 100g, uniformly mixing, standing, and filling when bubbles disappear.
EXAMPLE 2
[ FORMULATION ]
Figure BDA0001809890040000081
[ PREPARATION METHOD ] the same as in example 1.
EXAMPLE 3
[ FORMULATION ]
Figure BDA0001809890040000082
Figure BDA0001809890040000091
[ PREPARATION METHOD ] the same as in example 1.
The following is the pharmacodynamic study of the externally applied lauromacrogol gel of the invention:
the first step is that the bacterium killing (inhibiting) effect is as follows:
the microbiological bacteriostasis test shows that the aloe extract, the bacteriostat, the lauromacrogol, the bacteriostat and the lauromacrogol gel have obvious effect of killing (inhibiting) staphylococcus aureus, escherichia coli and pseudomonas aeruginosa. The results are shown in Table 1.
TABLE 1 bacteriostatic effect of the preparations of each group
Figure BDA0001809890040000092
The preparation of the lauromacrogol sample is described in example 1 above.
② the aloe extract and bacteriostatic agent sample preparation is as follows:
[ FORMULATION ]
Figure BDA0001809890040000101
[ PREPARATION METHOD ]
1. Weighing sodium alginate and aloe extract according to the formula ratio, adding 10g of glycerol, stirring to uniformly disperse the sodium alginate, adding 50g of water, and stirring to dissolve to obtain a first phase.
2. Weighing benzalkonium chloride, potassium sorbate, disodium hydrogen phosphate dodecahydrate and sodium dihydrogen phosphate dihydrate according to the formula, adding 10g of water, and stirring to dissolve to obtain phase II.
3. Mixing the first phase and the second phase respectively, stirring, adding water to 100g, mixing uniformly, standing until bubbles disappear, and filling.
③ the samples of the lauromacrogol and the bacteriostatic agent are prepared as follows:
[ FORMULATION ]
Figure BDA0001809890040000102
Figure BDA0001809890040000111
[ PREPARATION METHOD ]
1. Weighing lauromacrogol with formula ratio, adding 10g water, heating to 60 deg.C for dissolving to obtain phase I.
2. Weighing sodium alginate according to the formula ratio, adding 10g of glycerol, stirring to uniformly disperse the sodium alginate, adding 50g of water, and stirring to dissolve the sodium alginate to obtain phase II.
3. Weighing benzalkonium chloride, potassium sorbate, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and 10g of water according to the formula ratio, and stirring to dissolve to obtain a phase III.
4. Respectively adding the first phase and the third phase into the second phase, stirring, adding water to 100g, uniformly mixing, standing, and filling when bubbles disappear.
Secondly, healing time:
in order to understand the efficacy of the lauromacrogol gel on scalds, burns, abrasions and mosquito bites, aloe extract, bacteriostatic agent, lauromacrogol and bacteriostatic agent are used as reference medicaments according to the table 2, and the itching relieving effect and the healing time of the preparations in three groups on mosquito bites, the healing time of 1-2-degree burns and scalds, the pain relieving effect and the healing time of abrasions and sunburns are examined.
The three samples were used as follows: the pollution-free fresh wound surface can be directly coated without cleaning; the contaminated wound should be cleaned and then applied without any disinfectant.
From 2017, 60 patients suffering from mosquito bites are received, wherein 28 patients are male, and 34 patients are female; 30 patients with burn and scald are received totally, 1-2 degrees of burn are all adopted, wherein 11 cases are male, and 19 cases are female; a total of 30 patients with bruised sunburn, 17 in men and 13 in women; all the above cases were 4 years old at the minimum and 70 years old at the maximum.
TABLE 2 comparison of healing time of each group of preparations for mosquito bite, burn and scald
Figure BDA0001809890040000121
The result shows that the lauromacrogol gel provided by the embodiment of the invention has obvious effects of relieving itching and healing skin quickly for mosquito bites compared with aloe extract, bacteriostatic agent, lauromacrogol and bacteriostatic agent after being smeared to treat scalds, burns, abrasions and mosquito bites; can rapidly relieve pain and repair skin for burn and scald patients, and rapidly relieve pain, relieve itching and repair skin for sunburn and scratch patients.
Typical cases are:
case 1: when a certain horse is a female, the female is 28 years old and the ointment is burnt, the externally applied lauromacrogol gel of the invention example 1 is used for treating, the affected part is coated by the ointment, the skin does not bubble, and the wound is recovered as before after 1 week.
Case 2: when someone horse, a woman, is 31 years old and is bitten by mosquitoes, the externally applied lauromacrogol gel of the embodiment 1 of the invention is used for treating, the affected part is coated by the gel, and the itching can be relieved after about 1min after the gel is smeared. The skin redness and swelling of the affected part are eliminated the next day, and the affected part is recovered as before.
Case 3: when someone who is a male, is 29 years old and is abraded, the lauromacrogol external gel of the invention example 1 is used for treating the abrasion, and the drug is coated on the affected part, scabs quickly and has the efficacy of relieving pain and stopping bleeding.
Case 4: after a certain woman in 35 years old wears feet, the externally applied lauromacrogol gel for treating the foot abrasion in the embodiment 1 of the invention is used for treating the foot abrasion, the externally applied lauromacrogol gel is applied to an affected part for 6 times, has cool feeling, does not have any stabbing pain or uncomfortable feeling, is quick in wound scabbing, is continuously applied to the affected part after scabbing, is not dry and painful in the wound, and has better repairing effect.
Case 5: when a certain woman in age of 34 feels itchy due to skin allergy and mosquito bite, the externally applied lauromacrogol gel for treating the itching of the skin is used for treating the itching of the skin, the externally applied lauromacrogol gel for treating the itching of the woman is applied to an affected part for 4 times by using the externally applied lauromacrogol gel for treating the itching of the woman, and the itching relieving effect is better.
Case 6: when a certain person in Wei is burned by a man or a 50-year-old person at an age of I degrees, the externally applied lauromacrogol gel for treating the scald is applied to an affected part for 2 times, so that the pain relieving effect is good, the repairing function is good, and the skin can be quickly restored as before.
Case 7: when a child is 12 years old and faces are small pox-caused by mosquito bites, the externally applied lauromacrogol gel for treating the sassafras is used for treating the sassafras, the affected part is coated with the externally applied lauromacrogol gel for 3 times, itching can be relieved after about 1min after the externally applied lauromacrogol gel is coated for 3 times, the pox on the face is eliminated after the externally applied lauromacrogol gel is coated for 3 times, and the skin is recovered as before.
Case 8: when an arm is bitten by mosquitoes and allergic to some vermilion, the externally applied lauromacrogol gel of the embodiment 3 of the invention is used for treating, and the affected part is coated by the externally applied lauromacrogol gel for 4 times, so that the itching relieving and repairing effect is better.
Case 9: when a certain part of poplar is burnt by steam on the arm, the externally applied lauromacrogol gel for treating the arm is used for treating, 4 times of the affected part is coated by the externally applied lauromacrogol gel for treating the arm, the pain relieving effect is good, the repairing function is good, and the skin can be quickly restored as before.
The invention is not limited to the examples, and any equivalent changes to the technical solution of the invention by a person skilled in the art after reading the description of the invention are covered by the claims of the invention.

Claims (3)

1. The externally applied lauromacrogol gel is characterized in that:
the externally applied lauromacrogol gel is externally applied to the skin of burn, scald, sunburn, abrasion and mosquito bite, and comprises active ingredients of lauromacrogol, urea and aloe extract;
the weight parts of the active ingredients are as follows:
3-6 parts of urea;
3-5 parts of lauromacrogol;
0.5-4 parts of aloe extract.
2. The externally applied lauromacrogol gel of claim 1, wherein:
the externally applied lauromacrogol gel also comprises the following components in parts by weight:
0.1-0.4 part of benzalkonium chloride;
0.5-3 parts of sodium alginate;
0.1-0.4 part of potassium sorbate;
0.1-1 part of menthol;
5-15 parts of glycerol;
0.01-1.00 part of disodium hydrogen phosphate dodecahydrate;
0.01-1.00 part of dihydrate sodium dihydrogen phosphate;
the balance of purified water;
the total amount is 100 parts.
3. The method for preparing a lauromacrogol external gel as claimed in claim 2, wherein:
the method is realized by the following steps:
the method comprises the following steps: weighing lauromacrogol with formula ratio, adding 10-15 parts of purified water, heating to 60 deg.C for dissolving to obtain phase I;
step two: weighing sodium alginate and aloe extract according to the formula ratio, adding glycerol, stirring to uniformly disperse the components, adding 50-60 parts of purified water, and stirring to dissolve to obtain phase II;
step three: weighing benzalkonium chloride, potassium sorbate, urea, menthol, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate and 10-15 parts of purified water according to the formula ratio, and stirring for dissolving to obtain phase III;
step four: adding the phase III and the phase II into the phase I respectively, adding purified water to 100 parts, stirring uniformly, standing and filling.
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